Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373932 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A new series of compounds, 5-substituted 2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6(5H)-ones, have been designed and identified as potent and selective inhibitors of Hsp90. These compounds demonstrated nanomolar potency toward both Hsp90-regulated Her2 degradation and the growth of a panel of human tumor cell lines in cell-based assays. High selectivity of these compounds toward Hsp90 was evident given that they did not inhibit a panel of 34 kinases at 10 μM. The structure–activity relationship (SAR) of this series is reported here.
Graphical abstractThe discovery of a series of potent Hsp90 inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Xiaoyuan Li, Ellyn Shocron, Aimin Song, Neela Patel, Connie L. Sun,